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Cytochrome P450 1A2 (CYP1A2) Inhibitor Screening Kit (Fluorometric) (CAT#: CB-P237-K) Datasheet

Product Type
Cytochrome P450 1A2 (CYP1A2, EC is a member of the cytochrome P450 monooxidase (CYP) family of microsomal heterologous biological metabolic enzymes. CYP is the membrane-bound hemoglobin responsible for the phase I biotransformation reaction, in which lipophilic drugs and other heterogeneous biological compounds are converted into more hydrophilic products to promote human excretion. CYP1A2 is mainly expressed in liver, intestine and olfactory mucosa tissues, and catalyzes the oxidation of planar polycyclic aromatic and heterocyclic molecules (such as aromatic amines). CYP1A2 is responsible for about 10% of the metabolism of all small molecule drugs commonly used in humans. The polymorphism of the human CYP1A2 gene is associated with clinical drug/drug interactions involving widely used drugs, including methylxanthines (caffeine and theophylline), ciprofloxacin and many antidepressants and antipsychotics. Isoforms of the CYP1A subfamily are also involved in the metabolic activation of environmental carcinogens in cigarette smoke and combustion exhaust gas. Creative Biolabs' CYP1A2 inhibitor screening kit enables rapid screening of drugs and other new chemical entities (NCE) compound-CYP1A2 interactions in a reliable, high-throughput Fluorometric-based assay. This kit provides yeast microsomal preparations of human CYP1A2 and human cytochrome P450 reductase (CPR) enzymes. The assay utilizes a non-fluorescent CYP1A2 substrate, which is converted into a highly fluorescent metabolite detected in the visible light range (Ex / Em = 406/468 nm), thus ensuring a high signal-to-noise ratio. The interference of autoFluorometric is very small. The kit contains a complete set of reagents, enough to perform 100 reactions in a 96-well plate format.
100 assays

Figure 1 3-cyano-7-hydroxycoumarin (3-CHC) standard curve.

Figure 2 Reaction kinetics of recombinant human CYP1A2 enzyme at 37°C in the presence and absence of the indicated CYP1A2 inhibitors.

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